Potassium Carbonate → (R)-5-(6-Bromo-pyridin-2-yl)-2,5-dimethyl-2-trifluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-ylamine

Participants

Reaction Steps

A suspension of (R)-2-[(RS)-2-amino-2-(6-bromo-pyridin-2-yl)-propoxy]-3,3,3-trifluoro-2-methyl-propionitrile (0.688 g, 1.172 mmol), N-acetyl-L-cysteine (0.383 g, 2.344 mmol) and K2CO3 (0.356 g, 2.560 mmol) in abs. EtOH (4 ml) was stirred at 80° C. for 18 h. The reaction mixture was quenched with 10% aq. K2CO3 soln. and 3× extracted with TBME. The combined org. phases were washed with brine, dried over Na2SO4, filtered and concentrated to leave the title compound as a colourless solid. HPLC RtH4=0.68-0.70 min; ESIMS: 352, 354 [(M+H)+].

Provenance & Evidence